Disclosed are compounds of Formula (IIa),
wherein R
1
, R
2
, R
3A
, R
3B
, R
3C
, R
3D
, R
3E
, and R
4
are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa).
Isoxazole derivative as mutant isocitrate dehydrogenase 1 inhibitor
申请人:Daiichi Sankyo Company, Limited
公开号:US10040791B2
公开(公告)日:2018-08-07
It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R1, R2, R3, Y, and Z are as defined in claim 1.
研究发现,具有异噁唑骨架的通式(I)化合物对突变型 IDH1 蛋白具有极好的抑制活性,并能抑制该蛋白产生 2-HG,同时该化合物还能有效抑制表达该蛋白的各种肿瘤的生长。 式中,R1、R2、R3、Y 和 Z 如权利要求 1 所定义。
ISOXAZOLE DERIVATIVE AS MUTANT ISOCITRATE DEHYDROGENASE 1 INHIBITOR
申请人:Daiichi Sankyo Company, Limited
公开号:US20170313696A1
公开(公告)日:2017-11-02
It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R
1
, R
2
, R
3
, Y, and Z are as defined in claim
1.